Tumour targeting with radiometals for diagnosis and therapy

Chem Commun (Camb). 2013 May 25;49(42):4720-39. doi: 10.1039/c3cc41554f.

Abstract

Use of radiometals in nuclear oncology is a rapidly growing field and encompasses a broad spectrum of radiotracers for imaging via PET (positron emission tomography) or SPECT (single-photon emission computed tomography) and therapy via α, β(-), or Auger electron emission. This feature article opens with a brief introduction to the imaging and therapy modalities exploited in nuclear medicine, followed by a discussion of the multi-component strategy used in radiopharmaceutical development, known as the bifunctional chelate (BFC) method. The modular assembly is dissected into its individual components and each is discussed separately. The concepts and knowledge unique to metal-based designs are outlined, giving insight into how these radiopharmaceuticals are evaluated for use in vivo. Imaging nuclides (64)Cu, (68)Ga, (86)Y, (89)Zr, and (111)In, and therapeutic nuclides (90)Y, (177)Lu, (225)Ac, (213)Bi, (188)Re, and (212)Pb will be the focus herein. Finally, key examples have been extracted from the literature to give the reader a sense of breadth of the field.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / therapeutic use
  • Chelating Agents / therapeutic use
  • Humans
  • Neoplasms / diagnosis*
  • Neoplasms / drug therapy*
  • Neoplasms / metabolism
  • Radioisotopes / therapeutic use
  • Radiopharmaceuticals / therapeutic use*

Substances

  • Antineoplastic Agents
  • Chelating Agents
  • Radioisotopes
  • Radiopharmaceuticals